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Preparation method of pitavastatin calcium intermediate

A technology of pitavastatin calcium and intermediates, applied in the field of medicine, to achieve the effect of high yield

Inactive Publication Date: 2012-09-05
FOSHAN DAYI TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] The present invention aims at the problems existing in the preparation of pitavastatin calcium intermediates at present, and provides a kind of preparation method of pitavastatin calcium intermediates that solves the above problems

Method used

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  • Preparation method of pitavastatin calcium intermediate
  • Preparation method of pitavastatin calcium intermediate
  • Preparation method of pitavastatin calcium intermediate

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Embodiment Construction

[0028] As shown in the reaction flow formula 1, under the protection of nitrogen, add 300ml of tetrahydrofuran into a 2000ml reaction kettle, add 13.2g (0.33 moles) of 60% sodium hydride, cool to -10°C, and add 39.05% ethyl acetoacetate dropwise from the dropping funnel. g (0.3 moles), after the dropwise addition is complete, continue to stir for 30 minutes, dissolve 40.00 g (0.33 moles) of s-tert-butylsulfinamide in 100 ml of tetrahydrofuran, add it dropwise to the reaction kettle, stir and react for 40 minutes, and the reaction system After cooling to -20°C, 240 ml (0.48 mol) of 2 mol / liter n-butyllithium tetrahydrofuran solution was added dropwise from the dropping funnel, and the stirring reaction was continued for 1 hour. Dissolve (E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinoline-2-propenal 63.47g (0.2 mol) in 100ml tetrahydrofuran and add it dropwise to the reaction kettle In, continue stirring for 2 hours. 500ml of saturated ammonium chloride solution was added dropw...

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Abstract

The invention relates to the technical field of medicine, particularly a preparation method of a pitavastatin calcium intermediate, which comprises the following steps: in the process of synthesizing the pitavastatin calcium intermediate (E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-5-hydroxy-3-oxo-6-ethylheptenoate, reacting ethyl acetoacetate with s-sulfinyl amine to generate chiral imine, reacting with butyl lithium to generate chiral imido-enolate, and carrying out condensation reaction with (E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl-2-acraldehyde to obtain the intermediate s-(E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-5-hydroxy-3-oxo-6-ethylheptenoate with optical activity. The ee value is higher than 95%, the subsequent preparation of pitavastatin calcium does not need to remove inactive components by resolution, and the yield relative to the raw material is higher.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a pitavastatin calcium intermediate. Background technique [0002] Pitavastatin calcium, the chemical name is bis[(3R,5S,6E)-7-(2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy -6-heptenoic acid] monocalcium, the structural formula is as formula two: [0003] [0004] formula two [0005] Pitavastatin calcium, as a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, is clinically used to treat hyperlipidemia. It not only has the advantages of other statins, but also has a shorter onset time , The dosage is lower, the side effect is smaller, the tolerance is better, and it has a good market prospect. [0006] Usually, pitavastatin calcium is completed through the synthetic route of the following formula three: [0007] [0008] [0009] formula three [0010] As above, I ((E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinoli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/14
Inventor 唐良伟雍智全阴元魁雷安胜陈宝林
Owner FOSHAN DAYI TECH LTD
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